12,13-Dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (Arcyriaflavin A)

• Inhibitor of cdk4/cyclin D1 (IC₅₀ = 59 nM). Active against CaM kinase II (IC₅₀ = 25 nM) but displays selectivity over several other kinases in vitro (IC₅₀ values for inhibition of PKA and PKC are > 2 and > 100 μM respectively). Inhibits human cytomegalovirus (HCMV) replication in vitro (IC₅₀ = 200 nM).

OTAVAchemicals Catalogue Number: 7070707137
CAS Registry Number: 118458-54-1
Purity: 95%+ (HPLC)

Ref.: Zhu et al. Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. Bioorganic & Medicinal Chemistry Letters (2003), 13, 1231-1235

Abstract: A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H,14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC₅₀ of 69 nM. Compound 1d also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation.

DOI: 10.1016/s0960-894x(03)00133-1