Bommera Ravi Kumar, Kethireddy Shashikala, Govindapur Rajeshwar Reddy, Eppakayala Laxminarayana
Sreenidhi Institute of Science and Technology (Autonomous), Yamnampet, Ghatkesar, Hyderabad, Telangana, India.
Geethanjali College of Engineering and Technology, (Autonomous), Cheeryal, Keesara, Hyderabad, Telangana, India.
BMC Chem. 2021 May 4;15(1):30. doi: 10.1186/s13065-021-00757-y.
1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity.
A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a-j) were synthesized and their structures were confirmed by HNMR, CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231), lung cancer (A549) and prostate cancer (DU-145) by using MTT method. Among them, compounds 7a, 7b, 7c, 7d and 7i demonstrated more promising anticancer activity than standard.
Synthesized derivatives (7a-j) of 1,2,4-oxadiazole linked 5-fluorouracil and investigated for their anticancer activity towards a panel of four human cancer cell lines.
1,2,4-恶二唑衍生物在针对人类癌细胞系进行评估时表现出显著的抗癌活性。它们还具有抗炎、镇痛、抗糖尿病、免疫抑制、α,β受体拮抗剂、抗菌、抗蠕虫、组胺-H3和抗寄生虫特性。嘧啶类似物5-氟尿嘧啶是一种用于治疗多种实体恶性肿瘤的化疗药物。但其应用受到限制，因为它具有生物利用度低和毒性高等副作用。分子对接是一种典型工具，有助于识别靶点并设计具有高生物利用度和最低毒性的药物。
合成了一组1,2,4-恶二唑连接的5-氟尿嘧啶衍生物（7a-j），并通过HNMR、CNMR和质谱分析确认了它们的结构。此外，使用MTT法研究了这些化合物对四种人类癌细胞系（如MCF-7、MDA MB-231）、肺癌（A549）和前列腺癌（DU-145）的抗癌活性。其中，化合物7a、7b、7c、7d和7i表现出比标准药物更有前景的抗癌活性。
合成了1,2,4-恶二唑连接的5-氟尿嘧啶衍生物（7a-j），并研究了它们对四种人类癌细胞系的抗癌活性。
