Department of Biochemistry, Qauid-i-Azam University, Islamabad 45320, Pakistan.
Chem Biol Drug Des. 2012 Jun;79(6):950-9. doi: 10.1111/j.1747-0285.2012.01360.x. Epub 2012 Mar 19.
In continuation to our efforts in finding potential therapeutic agents, a variety of biologically significant semicarbazones were synthesized by the reaction of different carbonyl compounds with phenyl semicarbazides through microwave irradiation. Initially, 18 semicarbazones were studied for their antimicrobial, antitumor, and antioxidant potential. None of the tested compounds showed any antibacterial activity; however, some compounds showed significant antifungal activity. Interestingly, all compounds showed antitumor activity when tested against tumors grown on potato discs. These compounds were also tested for their effect on OH radical-induced oxidative DNA damage. All the compounds showed DNA protection to varying extent. Based on the promising results of antitumor and antioxidant activities, another set of 24 semicarbazones was synthesized, and all of these semicarbazones were evaluated for their antioxidant potential. The results showed that the semicarbazones derived from 2-nitrobenzaldehyde and acetophenone were the most active 2,2-diphenyl-1-picrylhydrazyl 9 (DPPH) free radical scavengers. The overall results have led to the identification of some interesting compounds which seem to have great potential to be developed into effective anticancer drugs.
为了寻找有潜力的治疗药物，我们通过微波辐射，使不同的羰基化合物与苯并脒反应，合成了多种具有生物意义的半卡巴腙。最初，我们研究了 18 种半卡巴腙的抗菌、抗肿瘤和抗氧化潜力。测试的化合物均没有表现出任何抗菌活性；然而，一些化合物表现出显著的抗真菌活性。有趣的是，所有化合物在测试对抗在土豆切片上生长的肿瘤时都表现出抗肿瘤活性。这些化合物还被测试了对 OH 自由基诱导的氧化 DNA 损伤的影响。所有化合物都在不同程度上显示出 DNA 保护作用。基于抗肿瘤和抗氧化活性的良好结果，我们又合成了另一组 24 种半卡巴腙，并评估了它们的抗氧化潜力。结果表明，由 2-硝基苯甲醛和苯乙酮衍生的半卡巴腙是最有效的 2,2-二苯基-1-苦基肼基（DPPH）自由基清除剂。总的结果表明，一些有趣的化合物具有很大的潜力，可以开发成为有效的抗癌药物。
