{"id":11613,"date":"2022-12-01T06:36:54","date_gmt":"2022-11-30T22:36:54","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11613"},"modified":"2022-12-01T06:36:54","modified_gmt":"2022-11-30T22:36:54","slug":"teng-qing-hus-team-published-research-in-journal-of-heterocyclic-chemistry-in-58-cas-13599-22-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11613","title":{"rendered":"Teng, Qing-Hu&#8217;s team published research in Journal of Heterocyclic Chemistry  in 58 | CAS: 13599-22-9"},"content":{"rendered":"<p>Teng, Qing-Hu published the artcile<b><i>Design, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives<\/i><\/b>,  <a href=\"https:\/\/www.ambeed.com\/products\/13599-22-9.html\">Computed Properties of  13599-22-9<\/a>,  the publication is  Journal of Heterocyclic Chemistry (2021), 58(8), 1656-1664, database is CAplus.<\/p>\n<p>According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives <strong>I<\/strong> (R<sup>1<\/sup> = 4-I, 3-Me, 4-Cl, etc.; R<sup>2<\/sup> = H, Me, Cl) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids <strong>II<\/strong> with secnidazole. The in vitro antitumor\/cytotoxicities activities against tumor and normal cell lines, including NCI-H460 (lung tumor cell), MCG-803 (gastric tumor cell), Skov-3 (ovarian tumor cell), BEL-7404 (liver tumor cell) and HL-7702 (normal liver cell), have been evaluated using MTT assay. All compounds <strong>I<\/strong> showed promising inhibitory activities against four tumor cell lines. The IC<sub>50<\/sub> of <strong>I<\/strong> (R<sup>1<\/sup> = 4-I; R<sup>2<\/sup> = H) against the BEL-7404 cell was 2.03\u03bcM, and those of <strong>I<\/strong> (R<sup>1<\/sup> = 3-Me; R<sup>2<\/sup> = H) against the NCI-H460, MCG-803 and Skov-3 were 1.34, 0.14, and 0.87\u03bcM, resp. All these values were much lower than those of the cisplatin. Furthermore, <strong>I<\/strong> (R<sup>1<\/sup> = 3-Me, R<sup>2<\/sup> = H; R<sup>1<\/sup> = 4-I, R<sup>2<\/sup> = H) were also verified to be considerably safe for normal human liver cell, since the lower IC<sub>50<\/sub> values than cisplatin. Based on these results, the cell cycle anal., apoptosis ratio detection and mitochondrial membrane potential assay of <strong>I<\/strong> (R<sup>1<\/sup> = 3-Me, R<sup>2<\/sup> = H; R<sup>1<\/sup> = 4-I, R<sup>2<\/sup> = H) were further performed aiming to investigate their inhibition mechanism of BEL-7404 cells. It is revealed that they have effectively inhibited the cell growth by arresting the BEL-7404 cells at S phase and induced apoptosis through the mitochondria-mediated pathway.<\/p>\n<p>Journal of Heterocyclic Chemistry published new progress about 13599-22-9. 13599-22-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid,Benzene, name is 1,5-Diphenyl-1H-pyrazole-3-carboxylic acid, and the molecular formula is C8H15ClN2, <a href=\"https:\/\/www.ambeed.com\/products\/13599-22-9.html\">Computed Properties of  13599-22-9<\/a>.<\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,<br \/><a href=\"Pyrazole - Wikipedia\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Journal of Heterocyclic Chemistry published new progress about 13599-22-9. 13599-22-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid,Benzene, name is 1,5-Diphenyl-1H-pyrazole-3-carboxylic acid, and the molecular formula is C8H15ClN2, <a href=\"https:\/\/www.ambeed.com\/products\/13599-22-9.html\">Computed Properties of  13599-22-9<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[819,131],"tags":[740],"class_list":["post-11613","post","type-post","status-publish","format-standard","hentry","category-13599-22-9","category-pyrazoles-derivatives","tag-m-w250-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - 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