145691-52-7

Upstream product

• 100-54-9 pyridine-3-carbonitrile 
• 626-39-1 1,3,5-trisbromobenzene 
• 100-48-1 pyridine-4-carbonitrile 

Downstream Products

• 145691-54-9 3-(3,5-dibromobenzyl)pyridine 
• 905917-32-0 (3-bromo-5-hydroxyphenyl)(pyridin-3-yl)methanone 
• 145691-58-3 3-Bromo-5-(pyridin-3-ylmethyl)benzaldehyde 
• 145691-97-0 ethyl 3-[3-(2-aminoethyl)-5-(pyridin-3-ylmethyl)phenyl]propanoate 
• 145691-81-2 3-[3-(2-ethoxycarbonylethyl)-5-(pyridin-3-ylmethyl)phenyl]propanoic acid 
• 145691-74-3 ethyl 3-[3-(2-ethoxycarbonylethyl)-5-(pyridin-3-ylmethyl)phenyl]propanoate 
• 145690-78-4 ethyl 3-{3-[2-(1-propylsulphonylamino)ethyl]-5-(pyridin-3-ylmethyl)phenyl}propanoate 
• 145691-89-0 ethyl 3-[3-(2-t-butoxycarbonylaminoethyl)-5-(pyridin-3-ylmethyl)phenyl]propanoate 
• 1026042-82-9 C₁₉H₂₃ClN₂O₄S 
• 145690-81-9 Ethyl 3-[3-(2-dimethylsulphamoylamino)ethyl-5-(3-pyridylmethyl)phenyl]propanoate 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of N -(3-(1 H -Indol-4-yl)-5-(2- methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent

The synthesis and optimization of a series of orally bioavailable 1-(1H-indol-4-yl)-3,5-disubstituted benzene analogues as antimitotic agents are described. A functionalized dibromobenzene intermediate was used as a key scaffold, which when modified by sequential Suzuki coupling and Buchwald-Hartwig amination provided a flexible entry to 1,3,5-trisubstituted phenyl compounds. A 1H-indol-4-yl moiety at the 1-position was determined to be a critical feature for optimal potency. The compounds have been shown to induce cell cycle arrest at the G2/M phase and demonstrate efficacy in both cell viability and cell proliferation assays. The primary site of action for these agents is revealed by their colchicine competitive inhibition of tubulin polymerization, and a computational model has been developed for the association of these compounds to tubulin. An optimized lead LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model.

ANTI-CANCER AGENTS ANS USES THEREOF

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula (I): and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3 R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6- 10 carbons in the ring portion, an optionally-substituted 6- membered heteroaryl group having 1- 3 nitrogen atoms in the ring portion, an optionally-substituted 5- membered heteroaryl group having 0- 4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6- membered ring is fused either to a 5- membered ring or to a 6- membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.

Anti-cancer agents and uses thereof

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.

Solid-phase synthesis of phenols and pyridinones via arylboronation/oxidation protocol using aryl bromides

A sequence of two known reactions, palladium catalyzed arylboronation of arybromide and subsequent oxidation of arylboronate with oxone, has been carried out to prepare functionalized phenols and pyridin-2(1H)-one which were later loaded on to resin for solid-phase synthesis. Using these resin-bound templates, a number of solid-phase methods were developed to generate libraries of substituted phenols and pyridin-2(1H)-one.

Thromboxane Modulating Agents. 3. lff-Imidazol-1-ylalkyl- And 3-Pyridinylalkyl-Substituted 3-[2-[(Arylsulfonyl)amino]ethyl]benzenepropanoic Acid Derivatives as Dual Thromboxane Synthase Inhibitor/Thromboxane Receptor Antagonists

The design of a series of dual thromboxane synthase inhibitor/thromboxane receptor antagonists based on a 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid thromboxane receptor antagonist template is described. Introduction of a 5-(lff-imidazol-l-ylme

Pyridine derived agents for cardiovascular diseases

STR1 Compounds of formula (I) or a biolabile ester thereof, or a pharmaceutically acceptable salt of either, wherein Rl, R2, R3 and R4 are each independently selected from H or C1 -C4 alkyl; R5 is (CH2)m SO2 R6, (CH2)m NHSO2 R6 or (CH2)m NHCOR7 ; R6 and R7 are C1 -C6 alkyl, C1 -C3 perfluoroalkyl(CH2)n, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R6 is NR8 R9 ; R8 is H or C1 -C4 alkyl; R9 is C1 -C6 alkyl, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring which may optionally incorporate a carbon-carbon double bond or a further hetero atom linkage selected from O, S, NH, N(C1 -C4 alkyl) and N(C1 -C5 alkanoyl), and which may optionally be substituted with one to three substituents each independently selected from C1 -C4 alkyl and C1 -C4 alkoxy, and which may optionally be benzo-fused; X is CH2, CHCH3, C(OH)CH3, C=CH2 or O; m is 0 or 1; n is 0, 1, 2 or 3; and Het is 3- or 4-pyridyl or 1-imidazolyl; with the proviso that when Het is 1-imidazolyl then X is CH2 or CHCH3, are combined thromboxane A2 synthetase inhibitors and thromboxane A2 /endoperoxide antagonists of utility in the treatment of disease conditions in which thromboxane A2 is a causative agent.