Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.

C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivatives 18 g and 9 c demonstrated 1000-fold and 1250-fold improvements, respectively, in the growth inhibition of HeLa cells compared to roscovitine (1).

Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I.

The introduction of an aryl ring onto the 4-position of the C-6 benzyl amino group of the Cdk inhibitor roscovitine (2), maintained the potent Cdk inhibition demonstrated by roscovitine (2) as well as greatly improving the antiproliferative activity. A series of C-6 biarylmethylamino derivatives was prepared addressing modifications on the C-6 biaryl rings, N-9 and C-2 positions to provide compounds that displayed potent cytotoxic activity against tumor cell lines. In particular, derivative 21h demonstrated a >750-fold improvement in the growth inhibition of HeLa cells compared to roscovitine (2).

Segregated assemblies in bridged electron-rich and electron-poor pi-conjugated moieties.

We report a general strategy for the spontaneous segregation of electron-rich and electron-poor pi-conjugated moieties using mutually phobic aliphatic fluorocarbon-hydrocarbon interactions.

Organic solar cells: an overview focusing on active layer morphology.

Solar cells constructed of organic materials are becoming increasingly efficient due to the discovery of the bulk heterojunction concept. This review provides an overview of organic solar cells. Topics covered include: a brief history of organic solar cell development; device construction, definitions, and characteristics; and heterojunction morphology and its relation to device efficiency in conjugated polymer/fullerene systems.