Boger, Dale L. published the artcileCC-1065 CBI analogs: an example of enhancement of DNA alkylation efficiency through introduction of stabilizing electrostatic interactions, Category: indole-building-block, the main research area is CC1065 CBI analog preparation DNA alkylation.
The three trimethylammonium salts I (R1 and R2 and R3 = H or NMe3+) proved to be 100 times more efficient at alkylating DNA than I (R1 and R2 and R3 = H) and exhibited DNA alkylation efficiencies identical to that of (+)-CC-1065. In addition, the agents I (R1 and R2 = H and R3 = NMe3+) and I (R1 and R3 = H and R2 = NMe3+) exhibited DNA alkylation selectivities identical to that of I (R1 and R2 and R3 = H). This may be attributed to spatially well-defined stabilizing electrostatic interactions between the pos. charged trimethylammonium salt lying on the peripheral face of the agents and the bracketing, neg. charged phosphates located in the DNA backbone that enhance the DNA noncovalent binding affinity without affecting DNA binding or alkylation selectivity. The agent I (R2 and R3 = H and R1 = NMe3+) exhibited an altered and more discriminating AT-rich adenine N3 alkylation selectivity than the other agents that may be attributed to the groove placement of the large trimethylammonium salt.
Bioorganic & Medicinal Chemistry published new progress about Biochemical alkylation. 136818-66-1 belongs to class indole-building-block, name is Methyl 6-nitro-1H-indole-2-carboxylate, and the molecular formula is C10H8N2O4, Category: indole-building-block.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles