{"id":10272,"date":"2022-10-20T01:52:11","date_gmt":"2022-10-19T17:52:11","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272"},"modified":"2022-10-20T01:52:11","modified_gmt":"2022-10-19T17:52:11","slug":"wang-les-team-published-research-in-acs-medicinal-chemistry-letters-in-2020-10-08-936250-20-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272","title":{"rendered":"Wang, Le’s team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3"},"content":{"rendered":"

Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3<\/a>, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.<\/p>\n

Herein we describe the discovery of A-1331852(I), a first-in-class orally active BCL-XL inhibitor that selectively and potently induces apoptosis in BCL-XL dependent tumor cells. This mol. was generated by re-engineering our previously reported BCL-XL inhibitor A-1155463 using structure-based drug design. Key design elements included rigidification of the A-1155463 pharmacophore and introduction of sp3-rich moieties capable of generating highly productive interactions within the key P4 pocket of BCL-XL. A-1331852 has since been used as a critical tool mol. for further exploring BCL-2 family protein biol., while also representing an attractive entry into a drug discovery program.<\/p>\n

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, HPLC of Formula: 936250-20-3<\/a>.<\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, HPLC of Formula: 936250-20-3<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[736,131],"tags":[716],"class_list":["post-10272","post","type-post","status-publish","format-standard","hentry","category-936250-20-3","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nWang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Wang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-19T17:52:11+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"1 minute\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272\",\"name\":\"Wang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-19T17:52:11+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10272#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Wang, Le’s team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. Pyrazole derivatives play an important role in antitumor agents.\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-US\"},{\"@type\":\"Person\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\",\"name\":\"Jessica.F\",\"image\":{\"@type\":\"ImageObject\",\"inLanguage\":\"en-US\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/\",\"url\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"contentUrl\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"caption\":\"Jessica.F\"}}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"Wang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives","description":"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272","og_locale":"en_US","og_type":"article","og_title":"Wang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives","og_description":"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-10-19T17:52:11+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"1 minute"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272","name":"Wang, Le's team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-10-19T17:52:11+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, HPLC of Formula: 936250-20-3, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=10272"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10272#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Wang, Le’s team published research in ACS Medicinal Chemistry Letters in 2020-10-08 | 936250-20-3"}]},{"@type":"WebSite","@id":"https:\/\/www.pyrazoles-derivatives.com\/#website","url":"https:\/\/www.pyrazoles-derivatives.com\/","name":"pyrazoles-derivatives","description":"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. Pyrazole derivatives play an important role in antitumor agents.","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-US"},{"@type":"Person","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1","name":"Jessica.F","image":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/","url":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","contentUrl":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","caption":"Jessica.F"}}]}},"_links":{"self":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/10272","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/users\/8"}],"replies":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=10272"}],"version-history":[{"count":0,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/10272\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=10272"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=10272"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=10272"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}