512787-45-0

Upstream product

• 512787-41-6 (5-nitro-1H-indol-1-yl)(phenyl)methanone 
• 6146-52-7 5-nitroindole 
• 98-88-4 benzoyl chloride 
• 65-85-0 benzoic acid 

Downstream Products

• 512787-50-7 N-(1-benzoyl-1H-indole-5-yl)-methanesulfonamide 
• 1350890-82-2 1-benzoyl-5-benzoylamino-4-bromo-1H-indole 
• 1350890-83-3 5-benzoylamino-4-bromo-1H-indole 
• 1350890-84-4 5-(benzoyl-tert-butoxycarbonylamino)-4-bromo-indole-1-carboxylic acid tert-butyl ester 
• 1350890-81-1 5-amino-1-benzoyl-4-bromo-1H-indole 

Relevant academic research and scientific papers

Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones

A small number of fluorinated 7-phenyl-pyrroloquinolinone (7-PPyQ) derivatives was synthesized in an attempt to improve the metabolic stability of 3N-ethyl-7-PPyQ and 3N-benzoyl-7-PPyQ. The possible impacts of the fluorine-hydrogen isosterism on both biol

Indole derivatives or salts thereof as well as preparation method and application of indole derivatives or salts thereof

The invention belongs to the technical field of chemical medicine, and relates to an Hh (Hedgehog) signal pathway Smoothed (SMO) receptor small molecule inhibitor, in particular to indole derivativesor salts thereof with Smoothed inhibitory activity, which are shown in chemical general formula (I) in the description, as well as a preparation method and pharmaceutical composition of the indole derivatives or salts thereof. Tests on inhibitory activity of Hh signal pathways show that most compounds have better inhibitory activity on the Hh signal pathways. The invention further discloses the application of the compounds to preparation of medicines for treating diseases associated with Hh, wherein the diseases are BCC (basal cell carcinoma), MB (medullblastoma), SCLC (small cell lung cancer), medulloblastoma, rhabdomyosarcoma, or a combination of the diseases.

Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents

A small library of 7-pyrrolo[3,2-f]quinolinones was obtained by introducing benzoyl, sulfonyl and carbamoyl side chains at the 3-N position, and their cytotoxicity against a panel of leukemic and solid tumor cell lines was evaluated. Most of them showed high antiproliferative activity with GI50s ranging from micro-to sub-nanomolar values, and these values correlated well with the inhibitory activities of the compounds against tubulin polymerization. Based on a recently proposed colchicine bind site inhibitors (CBSIs) pharmacophore, the interactions of the novel 7-PPyQs at the colchicine domain were rationalized. The most active compounds (4a and 4b) did not induce significant cell death in normal human lymphocytes, suggesting that the compounds may be selective against cancer cells. In particular, 4a was a potent inducer of apoptosis in both the HeLa and Jurkat cell lines. On the other hand, the sulfonyl derivative 4b exhibited a lower potency in comparison with 4a. With both compounds, induction of apoptosis was associated with dissipation of the mitochondrial transmembrane potential and production of reactive oxygen species, suggesting that cells treated with the compounds followed the intrinsic pathway of apoptosis.

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

The identification of an agent that is selectively activated by a cytochrome P450 (CYP) has the potential for tissue specific dose intensification as a means of significantly improving its therapeutic value. Towards this goal, we disclose evidence for the

1H-indole derivatives as a highly selective cyclooxygenase-2 inhibitor

The present invention relates to a novel 1H-indole derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor. Wherein, X, Y, and Q are defined in this specification respectively.