On November 27, 2003, Cai, Sui Xiong; Jiang, Songchun; Kemnitzer, William E.; Zhang, Hong; Attardo, Giorgio; Denis, Real published a patent.Related Products of 75629-62-8 The title of the patent was Preparation of substituted 4-aryl-4H-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and their uses against cancer and other disorders. And the patent contained the following:
The present invention is directed to substituted 4-aryl-4H-pyrrolo[2,3-h]chromenes and analogs thereof (shown as I; variables defined below; e.g. II). The present invention also relates to the discovery that compounds I are activators of caspases and inducers of apoptosis. Therefore, I can be used to induce cell death in a variety of clin. conditions in which uncontrolled growth and spread of abnormal cells occurs. The ability to activate the caspase cascade and induce apoptosis in human breast cancer cell lines T-47D and ZR-75-1 was measured for ∼50 examples of I, e.g. EC50 (nM) = 2.3 and 1.6, resp., for II. Although the methods of preparation are not claimed, ∼50 example preparations are included. For I: R1 = alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, aminoalkyl and oxiranylalkyl; R3 and R4 = H, halo, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, C1-10 alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitro, amino, cyano, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, carboxy, methylenedioxy, carbonylamido or alkylthio; R5 is H or C1-10 alkyl. A is (un)substituted and is aryl, heteroaryl, saturated carbocyclic, partially saturated carbocyclic, saturated heterocyclic, partially saturated heterocyclic or arylalkyl; D is (un)substituted and is a heteroaromatic, partially saturated (un)saturated heterocyclic fused ring, wherein said fused ring has 5 or 6 ring atoms, wherein one or two of said ring atoms are N atoms and the others of said ring atoms are C atoms. Y is CN, COR19, CO2R19 or CONR20R21, wherein R19, R20 and R21 = H, C1-10-alkyl, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl or aminoalkyl; or R20 and R21 are taken together with the N to form a heterocycle; and Z is NR22R23, NHCOR22N(COR23)2, N(COR22)(COR23), N:CHOR19 or N:CHR19 wherein R22 and R23 = H, C1-4 alkyl or aryl, or R22 and R23 are combined together with the group attached to them to form a heterocycle. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Related Products of 75629-62-8
The Article related to aryl pyrrolochromene analog preparation caspase activator apoptosis inducer, antitumor agent aryl pyrrolochromene analog preparation pharmaceutical composition, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 75629-62-8
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts