666259-67-2

Upstream product

• 666259-62-7 (4S)-3-{(2S)-2-[(5-methylindol-1-yl)methyl]pent-4-enoyl}-4-phenyl-1,3-oxazolidin-2-one 
• 666259-64-9 2-{(2S)-2-[(5-methylindol-1-yl)methyl]pent-4-enyl}-2-hydrocyclopenta[1,2-a]benzene-1,3-dione 
• 666259-61-6 (4S)-3-[3-(5-methylindol-1-yl)propanoyl]-4-phenyl-1,3-oxazolidin-2-one 
• 666259-65-0 (2R)-2-[(5-methylindol-1-yl)methyl]pent-4-enylamine 
• 666259-63-8 (2S)-2-[(5-methylindol-1-yl)methyl]pent-4-en-1-ol 
• 18108-86-6 3-(5-methylindol-1-yl)propanoic acid 
• 852715-08-3 N-{(2R)-2-[(5-methylindol-1-yl)methyl]pent-4-enyl}(2S)-3-carbamoyl-2-({[(fluoren-9-ylmethoxy)carbonylamino]cyclohexyl}carbonylamino)propanamide 
• 666259-66-1 N-{(2R)-2-[(5-methylindol-1-yl)methyl]pent-4-enyl} (2S)-2-amino-3-carbamoylpropanamide 

Downstream Products

• 666259-68-3 tert-butyl 3-[N-({N-[1-(N-{(2R)-2-[(5-methylindol-1-yl)methyl]pent-4-enyl}carbamoyl)(1S)-2-carbamoylethyl]carbamoyl}cyclohexyl)carbamoyl](3S,4S)-4-(4-{[bis(tert-butoxy)carbonyl]methyl}phenyl)hept-6-enoate 
• 852714-76-2 tert-butyl 2-[4-(1-{1-[N-({N-[1-(N-{(2R)-2-[(5-methylindolyl)methyl]-4-enyl}carbamoyl)-(1S)-2-carbamoylethyl]carbamoyl}cyclohexyl)carbamoyl]-(1S)-2-[(tert-butyl)oxycarbonyl]ethyl}-(1S)-prop-2-enyl)phenyl]propane-1,3-dioate 
• 852714-69-3 tert-butyl 3-[N-({N-1-(N-{(2R)-2-[(5-methylindolyl)methyl]pent-4-enyl}-(1S)-2-carbamoylethyl)carbamoyl}cyclohexyl)carbamoyl]-(3S,4S)-4-[4-nitrophenyl]hex-5-enoate 
• 857083-14-8 tert-butyl 3-[N-({N-1-(N-{(2R)-2-[(5-methylindolyl)methyl]pent-4-enyl}-(1S)-2-carbamoylethyl)carbamoyl}cyclohexyl)carbamoyl]-(3S,4S)-4-[4-(tert-butoxy)phenyl]hex-5-enoate 
• 852714-95-5 (3S,4S)-4-[4-(tert-Butoxy-methyl-phosphinoylmethyl)-phenyl]-3-(1-{(S)-2-carbamoyl-1-[(R)-2-(5-methyl-indol-1-ylmethyl)-pent-4-enylcarbamoyl]-ethylcarbamoyl}-cyclohexylcarbamoyl)-hex-5-enoic acid tert-butyl ester 
• 852714-87-5 (3S,4S)-4-[4-(Benzyl-tert-butoxy-phosphinoylmethyl)-phenyl]-3-(1-{(S)-2-carbamoyl-1-[(R)-2-(5-methyl-indol-1-ylmethyl)-pent-4-enylcarbamoyl]-ethylcarbamoyl}-cyclohexylcarbamoyl)-hex-5-enoic acid tert-butyl ester 
• 852714-80-8 2-{4-[(E)-(9S,10S,14R,18S)-18-Carbamoylmethyl-9-carboxymethyl-14-(5-methyl-indol-1-ylmethyl)-8,17,20-trioxo-7,16,19-triaza-spiro[5.14]icos-11-en-10-yl]-phenyl}-malonic acid 
• 852714-78-4 di-tert-butyl 2-[4-((9S,10S,18S,14R)-7,16,19-triaza-9-{[(tert-butyl)oxycarbonyl]methyl}-18-(carbamoylmethyl)-14-[(5-methylindolyl)methyl]-8,17,20-trioxospiro[5.14]icos-11-en-10-yl)phenyl]propane-1,3-dioate 
• 852714-70-6 tert-butyl 2-{(9S,10S,18S,14R)-7,16,19-triaza-18-(carbamoylmethyl)-14-[(5-methylindolyl)methyl]-10-(4-nitrophenyl)-8,17,20-trioxospiro[5.14]icos-11-ene-9-yl}acetate 
• 852714-71-7 tert-butyl 2-{(9S,10S,18S,14R)-7,16,19-triaza-10-(4-[(tert-butyl)oxycarbonylamino]phenyl)-18-(carbamoylmethyl)-14-[(5-methylindolyl)methyl]-8,17,20-trioxospiro[5.14]icos-11-en-9-yl}acetate 

Relevant academic research and scientific papers

SH2 domain binding inhibitors

Disclosed are compounds represented by the formula: [image] or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.

Synthesis of a 5-Methylindolyl-Containing Macrocycle That Displays Ultrapotent Grb2 SH2 Domain-Binding Affinity

The growth factor receptor-bound protein 2 (Grb2) is an SH2 domain-containing docking module that represents an attractive target for anticancer therapeutic intervention. Here, a ring-closing metathesis approach is utilized to synthesize a 5-methylindolyl