Jainey Pj, Bhat Ik
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences of Nitte University, Deralakatte, Mangalore, Karnataka, India.
J Young Pharm. 2012 Apr;4(2):82-7. doi: 10.4103/0975-1483.96621.
Nitrogen heterocyclic compounds such as pyrazolines have been found to possess a broad spectrum of biological activities such as anticancer, antitubercular, anti-inflammatory, analgesic, and antidepressant activities. Pyrazoline derivatives IV, V (a-e) have been synthesized from the intermediate chalcones III (a-h) by cyclizing with phenyl hydrazine and hydrazine hydrate. The structures of these compounds were confirmed by IR, NMR, and mass spectroscopy. Biological studies of the synthesized compounds showed promising antitumor, analgesic, and anti-inflammatory activities. The compounds were tested for their in vitro antitumor activity against EAC tumor cell lines. Compounds IVa and IVb showed the highest cytotoxicity of 80% at a 200 μg mL concentration. Among the tested compounds, IVa and Vd seem to be more effective analgesic agents. Compounds IVc, IVd, and Ve are found to be the most effective anti-inflammatory agents. Thus the results show that synthesized compounds possess antitumor, analgesic, and anti-inflammatory activity. It was observed that the test compounds with electron withdrawing groups (halogens) on the aromatic ring favors antitumor, analgesic, and anti-inflammatory activity.
已发现吡唑啉等氮杂环化合物具有广泛的生物活性，如抗癌、抗结核、抗炎、镇痛和抗抑郁活性。吡唑啉衍生物IV、V（a - e）由中间体查耳酮III（a - h）与苯肼和水合肼环化合成。这些化合物的结构通过红外光谱、核磁共振光谱和质谱得到证实。合成化合物的生物学研究显示出有前景的抗肿瘤、镇痛和抗炎活性。测试了这些化合物对艾氏腹水癌（EAC）肿瘤细胞系的体外抗肿瘤活性。化合物IVa和IVb在200μg/mL浓度下显示出最高80%的细胞毒性。在测试的化合物中，IVa和Vd似乎是更有效的镇痛剂。发现化合物IVc、IVd和Ve是最有效的抗炎剂。因此结果表明合成化合物具有抗肿瘤、镇痛和抗炎活性。据观察，在芳环上带有吸电子基团（卤素）的测试化合物有利于抗肿瘤、镇痛和抗炎活性。
