Shaik Afzal, Bhandare Richie R, Palleapati Kishor, Nissankararao Srinath, Kancharlapalli Venkata, Shaik Shahanaaz
Department of Pharmaceutical Chemistry Vignan Pharmacy College, Jawaharlal Nehru Technological University, Vadlamudi-522213, Andhra Pradesh, India.
Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, Ajman University, Ajman PO Box 346, UAE.
Molecules. 2020 Feb 26;25(5):1047. doi: 10.3390/molecules25051047.
Our previous work identified isoxazole-based chalcones and their dihydropyrazole derivatives as two important five-membered heterocycles having antitubercular activity. Hence, in the present study, we biologically evaluated 30 compounds, including 15 isoxazole ring-containing chalcones (-) and 15 dihydropyrazoles (-) derived from these chalcones for their antimicrobial, antioxidant, and anticancer activities. Chalcones exhibited superior antibacterial and antioxidant activities compared to dihydropyrazoles. Among the chalcones, compound showed potent antibacterial (MIC = 1 µg/mL) and antioxidant activities (IC = 5 ± 1 µg/mL). Dihydropyrazoles, on the contrary, demonstrated remarkable antifungal and anticancer activities. Compound (IC = 2 ± 1 µg/mL) showed excellent antifungal activity whereas two other dihydropyrazoles (IC = 2 ± 1 µg/mL) and (IC = 4 ± 1 µg/mL) exhibited potential anticancer activity. The compounds were also tested for their toxicity on normal human cell lines (LO2) and were found to be nontoxic. The active compounds that have emerged out of this study are potential lead molecules for the development of novel drugs against infectious diseases, oxidative stress, and cancer.
我们之前的工作确定了异恶唑基查尔酮及其二氢吡唑衍生物是两种具有抗结核活性的重要五元杂环化合物。因此，在本研究中，我们对30种化合物进行了生物学评估，其中包括15种含异恶唑环的查尔酮（-）以及由这些查尔酮衍生而来的15种二氢吡唑（-），以检测它们的抗菌、抗氧化和抗癌活性。与二氢吡唑相比，查尔酮表现出更优异的抗菌和抗氧化活性。在查尔酮中，化合物 显示出强效的抗菌活性（MIC = 1 µg/mL）和抗氧化活性（IC = 5 ± 1 µg/mL）。相反，二氢吡唑表现出显著的抗真菌和抗癌活性。化合物 （IC = 2 ± 1 µg/mL）显示出优异的抗真菌活性，而另外两种二氢吡唑 （IC = 2 ± 1 µg/mL）和 （IC = 4 ± 1 µg/mL）表现出潜在的抗癌活性。这些化合物还针对正常人类细胞系（LO2）进行了毒性测试，结果发现它们无毒。本研究中筛选出的活性化合物是开发抗传染病、氧化应激和癌症新药的潜在先导分子。
