Synthesis Characterization and Biological Investigation of New Bioactive Heterocyclic Compounds

Abstract

Mainstream cancer research has continued to place a significant emphasis on the newlinedevelopment of new and effective therapeutic candidates to tackle rising treatment newlineresistance and off-target toxicities. Here, a series of novel 3-(substitutedphenyl) -2-(4- newline(substitutedphenyl) thiazol-2-yl) -2H-pyrazolo[3,4-d] thiazol-5(6H)-one derivatives were newlinesynthesized and characterized. The ability of the synthesized compounds to reduce the newlinesurvival of the human breast cancer cell line MDA-MB 231 was evaluated. When newlinecompared to the reference chemical, 5-fluorouracil, 5b, and 5i showed the highest newlineinhibitory activity (IC50: 550 ± 0.78 and#956;M and 504 ± 0.89 and#956;M respectively) on the viability newlineof MDA-MB 231 cells. To find more powerful drugs, molecular docking analyses have newlinebeen carried out. newlineChapter-2 newlineThe creation of novel and potent therapeutic options has continued to get considerable newlineattention in mainstream cancer research in an attempt to fight growing toxicity and offtarget newlinetoxicity rates and rising treatment resistance Here, a series of novel 4- newline(substitutedphenyl)-8-(4-chlorophenyl)-3-methyl-6-oxo-1,6-dihydropyrazolo[3,4-d] newlinepyrimido[1,2-a]pyrimidine-7-carbonitrile derivatives were synthesized and characterized. newlineThe capacity of the synthesized compounds to decrease the survival of the human breast newlinecancer cell line MDA-MB 231 was studied. When compared to the reference chemical, 5- newlinefluorouracil, compound 6b showed the highest inhibitory activity (IC50: 370 ± 0.24 and#956;M) newlineon the viability of MDA-MB 231 cells. To find more powerful drugs, molecular docking newlineanalyses have been carried out. newlineABSTRACT newlineSchool of Chemical Science S.R.T.M. University, Nanded. Page 2 newlineChapter-3 newlineIn a one-pot, four-component cyclocondensation reaction, a new class of 3- newline(substitutedphenyl)-5-oxo-3,4,5,6-tetrahydroimidazo[4,5-c]pyrazole-2(1H)-carbaldehyde newlinederivatives was synthesized (5a-l) employing the catalytic Beaching Earth Clay (pH 12.5 newlinewt %) and PEG-400 as a green solvent. Spectral data were used to confirm the structures newlineof all the synthesized compounds. The ta