Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C9H7NO2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1670-82-2
Design, synthesis, and biological evaluation of indole carboxylic acid esters of podophyllotoxin as antiproliferative agents
A series of indole carboxylic acid conjugates of the podophyllotoxin were synthesized and evaluated as antiproliferative agents against two human chronic myeloid leukemia cell lines. Several compounds (In-2, In-8 and In-9) not only showed antiproliferative activity against normal K562 cells but also exhibited potent antineoplastic effect against resistant K562/VCR cells. The indole-6-formyl conjugate, In-9, revealed potent cytotoxic activity against K562 and K562/VCR cell lines, with IC50 values of 0.100 ¡À 0.008 and 0.227 ¡À 0.011 muM, respectively. Preliminary mechanism studies indicated that In-9 could disrupt the microtubule network in K562/VCR cells via occupying the colchicine binding site of the tubulin. Molecular dynamics simulation results revealed that the complex of In-9 and tubulin were stable. Furthermore, In-9 induced intracellular ROS generation, apoptosis, and cycle arrest at the G2 phase by inhibition of CDKs, loss of mitochondrial membrane potential and cleavage of caspase. In-9 simultaneously induced K562/VCR cells autophagy by upregulating the levels of Beclin1 and LC3-II, and exhibited anti-MDR ability by downregulating the levels of P-gp and MRP1. Finally, In-9 activated the AMPK and JNK signaling, and inhibited the ERK, P38, and PI3K/AKT/mTOR signaling in K562/VCR cells. In silico prediction indicated that In-9 mainly obeyed Lipinski rule for druglikeness. Together, In-9 possessed potent antiproliferative activity, and may be a promising agent for the potential treatment of resistant leukemia cancer.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.COA of Formula: C9H7NO2, you can also check out more blogs about1670-82-2
Reference£º
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