308110-69-2

Upstream product

• 241470-53-1 2-bromo-10H-indolo[3,2-b]quinoline-11-carboxylic acid 
• 91-56-5 indole-2,3-dione 
• 87-48-9 5-Bromo-1H-indole-2,3-dione 
• 118-92-3 anthranilic acid 
• 612-42-0 phenylglycine-o-carboxylic acid 
• 16851-69-7 2-(N-(carboxymethyl)acetamido)benzoic acid 
• 16800-67-2 N,O-diacetylindoxyl 
• 874212-39-2 (Z)-3-Chloro-3-(2-nitro-phenyl)-propenal 
• 33588-54-4 5-bromoindoxyl diacetate 
• 577-59-3 2-acetylnitrobenzene 
• 874212-44-9 6-bromo-2-(2-nitro-phenyl)-quinoline 

Relevant academic research and scientific papers

A novel inhibitor of human telomerase derived from 10h-indolo[3,2-b]quinoline

The bis-dimethylaminoethyl derivative of quindoline (10H-indolo[3,2-b]quinoline), an alkaloid from the West African shrub Cryptolepis sanguinolenta, has been synthesised. This has been shown to have modest cytotoxicity, as well as inhibitory activity agai

Synthesis and biological evaluation of indoloquinoline alkaloid cryptolepine and its bromo-derivative as dual cholinesterase inhibitors

Alkaloids have always been a great source of cholinesterase inhibitors. Numerous studies have shown that inhibiting acetylcholinesterase as well as butyrylcholinetserase is advantageous, and have better chances of success in preclinical/ clinical settings. With the objective to discover dual cholinesterase inhibitors, herein we report synthesis and biological evaluation of indoloquinoline alkaloid cryptolepine (1) and its bromo-derivative 2. Our study has shown that cryptolepine (1) and its 2-bromo-derivative 2 are dual inhibitors of acetylcholinesterase and butyrylcholinesterase, the enzymes which are involved in blocking the process of neurotransmission. Cryptolepine inhibits Electrophorus electricus acetylcholinesterase, recombinant human acetylcholinesterase and equine serum butyrylcholinesterase with IC50 values of 267, 485 and 699 nM, respectively. The 2-bromo-derivative of cryptolepine also showed inhibition of these enzymes, with IC50 values of 415, 868 and 770 nM, respectively. The kinetic studies revealed that cryptolepine inhibits human acetylcholinesterase in a non-competitive manner, with ki value of 0.88 μM. Additionally, these alkaloids were also tested against two other important pathological events of Alzheimer's disease viz. stopping the formation of toxic amyloid-β oligomers (via inhibition of BACE-1), and increasing the amyloid-β clearance (via P-gp induction). Cryptolepine displayed potent P-gp induction activity at 100 nM, in P-gp overexpressing adenocarcinoma LS-180 cells and excellent toxicity window in LS-180 as well as in human neuroblastoma SH-SY5Y cell line. The molecular modeling studies with AChE and BChE have shown that both alkaloids were tightly packed inside the active site gorge (site 1) via multiple π-π and cation-π interactions. Both inhibitors have shown interaction with the allosteric “peripheral anionic site” via hydrophobic interactions. The ADME properties including the BBB permeability were computed for these alkaloids, and were found within the acceptable range.

Antifungal and antiparasitic indoloquinoline derivates

A compound having the formula: wherein: R is an electron withdrawing or electron donating moiety; R5 and R10 may be the same or different and are a straight or branched 1-5 carbon or heteroatom chain substituted terminally by a cycloalkyl or aromatic ring, or other structural isomer or complex thereof; n is the position of substitution of R; Z is N—R10, O, S, S═O, CH2 or C═O; y is 1-5 and Q is Z or NH, with the proviso that, where Z is NH, N—CH3, S or O and Rn is H, R5 may not be CH3; as well as quaternary ammonium salts thereof and their use as pharmacological compositions and for methods of treatment.

Thermal cyclization of 3-arylamino-3-(2-nitrophenyl)-propenal Schiff base hydrochlorides followed by triethyl phosphite mediated deoxygenation: A facile synthesis of quindolines

A simple and useful method for the synthesis of various 2-substituted quindolines starting from 2-nitroacetophenone is described.

Substituted indoloquinolines as new antifungal agents.

Cryptolepine (2) possesses desirable properties to serve as a lead in developing new antifungal agents. Using SAR techniques, several analogues of cryptolepine were designed to increase potency and to broaden the antifungal spectrum over several opportuni

Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents

The indoloquinoline alkaloid cryptolepine 1 has potent in vitro antiplasmodial activity, but it is also a DNA intercalator with cytotoxic properties. We have shown that the antiplasmodial mechanism of 1 is likely to be due, at least in part, to a chloroqu