Antimycobacterial and anticancer activity of newly designed cinnamic acid hydrazides with favorable toxicity profile
نویسندگان
چکیده
A series of twelve novel hybrids cinnamic acid and thiocarbohydrazones were designed, synthesized in high yield using a simple coupling strategy via chlorides, evaluated for their impact against Mycobacterium tuberculosis (Mtb) cancer cells survival. Among them, compound 3 demonstrated strong anti-Mtb activity by reducing bacilli survival for>90 % all three treated Mtb isolates, whereas isoniazid rifampicin did not. Moreover, didn’t affect vitality HepG-2 cells, implying on advantageous hepatotoxicity profile compared to current therapeutic options tuberculosis. Compounds 2a 3b displayed as inducers apoptosis A549 both activating intrinsic caspase pathway cell cycle arrest at the G0/G1 phase. Subsequent analyses disclosed differences activities, where has ability induce production mitochondrial superoxide anions, while significantly inhibited cellular mobility. More importantly, considerably affected viability HaCaT had moderate only later. Molecular modeling studies indicated permeability good absorption through human intestine, aqueous solubility with poor blood–brain barrier permeability. In summary, our results reveal that compounds represent promising agents treatment, respectively, indicating further investigation needs be performed clarify mechanisms anticancer activity.
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ژورنال
عنوان ژورنال: Arabian Journal of Chemistry
سال: 2022
ISSN: ['1878-5379', '1878-5352']
DOI: https://doi.org/10.1016/j.arabjc.2021.103532