Synthesis and evaluation of antitumor activity of novel N-acyllavendamycin analogues and quinoline-5,8-diones

Abstract

A series of 7-N-acyllavendamycins with zero, one or two substituents at the C-2', C-3', and C-11' were synthesized through short and efficient methods. Pictet-Spengler condensation of 7-N-acylamino-2-formylquinoline-5,8-diones with tryptamine or tryptophans produced the desired lavendamycins. Screening data on a panel of three ras oncogene-transformed cell lines and the non-transformed parent cell line showed that a significant number of these analogues are potent antitumor agents and appear to be particularly active against K-ras transformed cells. Compared with the corresponding quinolinediones, these novel lavendamycins are much more inhibitory toward the transformed cells indicating that the beta-carboline moiety of the lavendamycin analogues plays an important role in its potency and selective toxicity.

Molecular Docking and Biological Evaluation of Functionalized benzo[h]quinolines as Colon Cancer Agents

“…Molecules with quinoline skelon are reported as anti-inflammatory, antimalarial, antiasthmatic, antihypertensive, antibacterial and platelet derived growth factor receptor tyrosine kinase (PDGF-RTK) inhibiting agents [6]. Various quinoline derivatives are reported to display considerable anticancer activities [7][8]. Quinoline skeleton act as anticancer agents through several mechanisms for example; inhibition of topoisomerase [9], cell cycle arrest in the G2 phase [10], and tubulin polymerization inhibition [11].…”

Small molecule PZL318: forming fluorescent nanoparticles capable of tracing their interactions with cancer cells and activated platelets, slowing tumor growth and inhibiting thrombosis

“…13 Other effects on cells and organs include modulating the extrinsic or death receptor pathway and the intrinsic or mitochondrial pathway, 14 interfering with Ras-related signaling pathways, 15 inhibiting tumor-related enzymes, [16][17][18][19] and limiting thrombosis and inflammation. [20][21][22] Inflammation is a wellrecognized and critical component of the tumor progression, 23,24 and thromboembolism is a leading cause of cancer patient death.…”

Design and synthesis of some novel quinoline derivatives as anticancer and radiosensitizing agents targeting VEGFR tyrosine kinase

“…Also, several novel quinoline derivatives have been reported to show substantial anticancer activities [7][8][9][10][11][12][13][14].…”