Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
Eur J Med Chem. 2011 Dec;46(12):5763-8. doi: 10.1016/j.ejmech.2011.08.015. Epub 2011 Aug 16.
Eight novel 2-pyrazolines (2a-h) were synthesized by the reaction of appropriate chalcones/flavanones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anti-inflammatory and anti-cancer activities. Two compounds 2c and 2e showed good anti-inflammatory activity which is comparable to the reference drug celecoxib in carrageenan-induced rat paw edema bioassay and found safe from the point of view of ulcer induction. Compounds 2c and 2e showed very mild inhibition against the enzymatic activity of ovine COX-1 and COX-2 (in vitro). The compounds 2c and 2f exhibited considerable antitumor activity against tested 60 human tumor cell lines. Specifically, compound 2f exhibited promising anti-proliferative activity with GI(50) values less than 2 μM particularly against MOLT-4 (1.94), SR (1.28) in leukemia cancer, EKVX (1.88) in non small cell lung cancer, COLO 205 (1.69) in colon cancer.
合成了 8 种新型 2-吡唑啉（2a-h），通过适当的查尔酮/黄烷酮与 4-肼基苯磺酰胺盐酸盐反应得到，并测试了其抗炎和抗癌活性。两种化合物 2c 和 2e 表现出良好的抗炎活性，在角叉菜胶诱导的大鼠足肿胀生物测定中与参比药物塞来昔布相当，并且从溃疡诱导的角度来看是安全的。化合物 2c 和 2e 对绵羊 COX-1 和 COX-2 的酶活性（体外）表现出非常轻微的抑制作用。化合物 2c 和 2f 对测试的 60 个人类肿瘤细胞系表现出相当的抗肿瘤活性。具体而言，化合物 2f 表现出有希望的抗增殖活性，GI（50）值小于 2 μM，特别是对白血病癌症中的 MOLT-4（1.94）、SR（1.28），非小细胞肺癌中的 EKVX（1.88），结肠癌中的 COLO 205（1.69）。
