Kewal Kumar

Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from β-lactams and 7-chloroquinoline using click chemistry

1,2,3-Triazole tethered β-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and evaluated as potential antimalarial agents. Activity against cultured Plasmodium falciparum was dependent on the N-substituent of the β-lactam ring as well as the presence of bis-triazole at the C-3 position. The observed activity profiles were further substantiated by docking studies via inhibition of P. falciparum dihydrofolate reductase (PfDHFR), a potential target for the development of new anti-malarials.

Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil–isatin conjugates and their cytotoxic evaluation

The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC(50) values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines.

Prodigiosin alkaloids: recent advancements in total synthesis and their biological potential

Despite recent developments in combinatorial chemistry and related techniques for facilitating drug discovery and development, natural products continue to play a prominent and evolving role for the development of new therapeutic agents. Pyrrole containing natural products constitute an integral part of this strategy. The structure and reactivity of pyrrole along with its propensity to polymerize renders it a relative speciality and certainly not something for the faint of heart. Besides, the well known tetrapyrrolic “Pigments of life,” other fascinating natural products incorporating multiple copies of the pyrrole ring system are attracting the attention of organic medicinal chemists and must be acknowledged.

Highly potent anti-proliferative effects of a gallium(III) complex with 7-chloroquinoline thiosemicarbazone as a ligand: Synthesis, cytotoxic and antimalarial evaluation

A gallium(III) complex with 7-chloroquinoline thiosemicarbazone was synthesized and characterized. The complex proved to be thirty-one times more potent on colon cancer cell line, HCT-116, with considerably less cytotoxicity on non-cancerous colon fibroblast, CCD-18Co, when compared to etoposide. Its anti-malarial potential on 3D7 isolate of Plasmodium falciparum was better than lumefantrine.

Synthesis and antiprotozoal activity of mono- and bis-uracil isatin conjugates against the human pathogen Trichomonas vaginalis

A library of mono- and bis-uracil isatin conjugates were synthesized and subjected for the assessment of their in vitro activity against the protozoal pathogen Trichomonas vaginalis. The structure activity studies (SAR) revealed that the bis-uracil-isatin based conjugates were more effective than their corresponding mono conjugates in inhibiting the growth of T. vaginalis at approximately 10 μM with no visual effect on mammalian cells at the same concentration.

1H-1,2,3-Triazole-Tethered Uracil-Ferrocene and Uracil-Ferrocenylchalcone Conjugates: Synthesis and Antitubercular Evaluation

Copper‐catalyzed azide‐alkyne [3 + 2] cycloaddition has been utilized for preparing a series of 1H‐1,2,3‐triazoles with the purpose of probing structure–activity relationships among a uracil‐ferrocene‐triazole conjugate family. The antitubercular evaluation studies revealed an improvement in activity with the introduction of a ferrocene nucleus among N‐alkylazido‐uracil precursors, with a preference for a bromo‐substituent along with moderate chain lengths of n = 2–6. The reported protocol is a successful approach for integrating uracil‐ferrocene‐chalcone functionalities tethered via 1H‐1,2,3‐triazole rings with apparent physicochemical stability.