Background: A series of novel 2 substituted 4-anilinoquinazolines-pyrrole hybrids were synthesized, and cytotoxic activity were evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay. Methods: The cell line used for the activity was MCF-7 breast cancer cell line and A459 human lung adenocarcinoma cell line. The newly quinazoline-pyrrole hybrid compounds have been synthesized from the 4chloro-7-(3-chloropropoxy)-6-methoxy-2-phenylquinazoline derivatives. The chemical structure of the synthesized compounds has been confirmed by FTIR, 1 HNMR, 13 C NMR, and mass spectral data. The cytotoxic study was conducted using morphological study and MTT assay against adenocarcinoma and human breast cancer cell lines. Results: The results of cytotoxic evaluation revealed that few compounds show moderate to promising activity when compared with standard doxorubicin (IC 50 value 41.05 μM at 72 h). The synthesized compounds 7d and 7f were found effective in breast cancer cell line with IC 50 values 40.64 μM and 44.98 μM at 72 h, respectively. The synthesized compounds 7d, 7f, 7g, and 7h were found effective in adenocarcinoma cell line with IC 50 values of 41.05 μM, 45.54 μM, 46.93 μM, and 48.62 μM, respectively. Conclusion: Based on the experimental evidences, we proposed structure activity relationship to provide significant information for the design and development of further potent anticancer agents.
Cancer is one of the leading causes of death worldwide and accounts for almost 13% deaths than any other infectious diseases (Thun et al., 2010). According to World Health Organization (WHO), projections of cancer prevalence is expected to raise by 21.7 million cases of oncological patients and 13 million deaths by 2030 (El-Azab et al., 2017; Boussari et al., 2018). With the increase in prevalence of cancer and thereby rapidly escalating costs, there are still types of cancer with massive unmet medical needs (Kummar and Takimoto, 2018). Therefore, the development of novel chemotherapeutic agents to fight against this deadly disease is needed urgently (Chakraborty and Rahman, 2012). Nitrogen containing heterocyclic compounds like quinolines and pyridines core rings plays a very important role in drug discovery and development on cancer. (Taylor et al., 2016; Jabir et al., 2018) Some of the marketed drugs have core structure of quinazoline which includes Afatinib (I,
Based on the literature review, we have found that Isatin-Oxadiazole derivatives are exhibiting different activities like anti-oxidant, antiviral, anti-microbial and anti-convulsant and we synthesized Isatin-Oxadiazole hybrids. Among the series of compounds (E)-5-chloro-3,(2,(5-mercapto-1,3,4-oxadiazol-2yl)hydrazono)-indolin-2-one(IVb), (E)-5-bromo-3,(2,(5-mercapto-1,3,4-oxadiazol-2-yl)hydrazono)indolin-2-one(IVe) showed most significant antioxidant activity.
An efficient synthetic approach of pharmacologically important diversely functionalized compounds (Triazoles and Tetrazoles) through the cycloaddition of Glucals, Azides and nitriles in presence of CuII(OTf) as a catalyst by conventional and microwave methods and to compare the yields. The antibacterial activity of the triazoles and tetrazole were tested by serial dilution method taking drug at a concentration of 150 mg/ml. The anti-fungal activies of the triazoles and tetrazole were tested by agar diffusion method (cup-plate method) taking drug at a concentration of 100 mg/ml and 150 mg/ml against five fungi (C.albicans, C.rugosa, S.cerevisiae, A.flavus and A.niger).
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