V. Devaiah

Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

Quinoxaline, quinazoline and benzimidazole based templates have been synthesized on solid-support employing different methodologies. This review enlightens academic and industrial examples of combinatorial synthesis for this type of heterocycles that appeared in the literature in the last decade. Hence, some of the important synthetic strategies for the generation of quinoxaline, quinazoline and benzimidazole based privileged structures, and the important biological activities for these heterocycles have been highlighted. Further, benzothiadiazinone, thioxoquinazolinone, cinnoline and indazole are also examined in this review.

Solid-phase synthesis of new pyrrolobenzodiazepine-chalcone conjugates: DNA-binding affinity and anticancer activity.

A new class of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-chalcone conjugates have been prepared by employing a solid-phase synthetic protocol. In this strategy an intramolecular aza-Wittig reductive cyclization approach has been utilized. Interestingly, some of these molecules have shown enhanced DNA-binding affinity and promising anticancer activity on a large number of human cancer cell lines.

Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Benzodiazepine Based Privileged Structures

Benzodiazepine based heterocycles can be prepared efficiently on solid-support by employing different approaches. In this review, an effort has been made to highlight academic and industrial examples of combinatorial synthesis for this type of heterocycles published in the last decade. Therefore, it describes synthetic strategies for the generation of benzodiazepine privileged structures employing the corresponding resin-bound substrates. Further, the most relevant biological properties of these heterocycles have also been incorporated.

Facile reduction of aromatic nitro/azido functionality on solid support employing Al/NiCl2.6H2O and Al/NH4Cl: synthesis of pyrrolo[2,1-c][1,4]benzodiazepines

Abstract An efficient and mild method for the reduction of aromatic nitro and azido groups on solid support using Al/NiCl 2 ·6H 2 O and Al/NH 4 Cl is described. This solid phase reduction technique has been applied towards the synthesis of DNA binding pyrrolo[2,1- c ][1,4]benzodiazepine antitumour antibiotics.

Synthesis and Biological Activity of C-8 Fluoroaryl Substituted Pyrimidine Linked-Pyrrolobenzodiazepine Conjugates

Synthesis of C-8 fluoroaryl substituted pyrimidine linked-PBD conjugates are described. The compounds are prepared with varying degrees of linker length in order to probe the structural requirements for optimal in vitro antitumour activity. These compounds have been tested against a panel of 60 human cancer cell lines, and it is demonstrated that compound 5b with four carbon spacer exhibited promising in vitro anticancer activity in comparison to the other analogues (5a and 5c).