Design, synthesis and cytotoxicity of chimeric erlotinib-alkylphospholipid hybrids
Two series of erlotinib-alkylphospholipid hybrids were prepared and evaluated for their antiproliferative activities against a panel of four cell lines representing lung, breast, liver and skin cancers using erlotinib and miltefosine as reference standards. Amide analogs elicited more enhanced cytotoxic activity than analogous esters. Amide derivatives 8d and 8e exhibited promising broad-spectrum antiproliferative activity and higher efficacy than reference erlotinib and miltefosine. Their cellular GI50 values was in the ranges of 24.7–46.9 μM and 26.8–43.1 μM for 8e and 8d respectively. Assay results of the inhibitory activity of the prepared compounds on EGFR kinase reaction and Akt phosphorylation in conjugation with statistical correlation analysis indicated that other mechanisms might contribute to their elicited cytotoxicities. In addition, statistical correlation analysis revealed that mechanisms of elicited cytotoxicities for amide series might be different from ester series. In addition, correlation analysis indicated variations in the mechanisms according to the types of cell line.
Alam, Md. Maqusood,Hassan, Ahmed H.E.,Lee, Kun Won,Cho, Min Chang,Yang, Ji Seul,Song, Jiho,Min, Kyung Hoon,Hong, Jongki,Kim, Dong-Hyun,Lee, Yong Sup
supporting information
p. 51 - 62
(2018/11/27)
Antihypertensive phosphate derivatives
Antihypertensive phosphate derivatives having the following formula are described: STR1 wherein X is a C1 -C24 branched or straight chain alkyl group; R is selected from the group consisting of hydrogen and C1 -C4 alkyl, with the proviso that at least one R group is not hydrogen; T is selected from the group consisting of hydrogen and STR2 wherein R1 is selected from the group consisting of hydrogen, C1 -C4 branched or straight chain alkyl, C1 -C4 branched or straight chain alkoxy and C1 -C4 branched or straight chain alkylamino; Q is a bivalent radical selected from the group consisting of --(CH2)p -- and --(CHR1)p --, wherein p is an integer from 2 to 12 and the moiety --(CHR1)p -- represents an alkylene chain which is substituted by one or more C1 -C10 alkyl groups or phenyl groups; Z is selected from the group consisting of STR3 wherein R2 may be chain alkyl and q is an integer from 4 to 7; in either the racemic or in the optically active form.
-
(2008/06/13)
Structure-Activity Relationship in PAF-acether. 3. Hydrophobic Contribution to Agonistic Activity
The synthesis of some selected PAF-acether homologues with an alkoxy-chain length from C1 to C20 in position 1 is described.All agonist activities are closely correlated among themselves and with the calculated fatty-chain hydrophobicity.After a discussio
Phosphocholine derivatives having antihypertensive action
Phosphocholine derivatives and compositions are described which are useful as hypotensive agents and in the treatment of hypertension in warm-blooded animals.
-
(2008/06/13)
Synthesis of platelet activating factor (PAF) via a cyclic tin intermediate
-
Marx,Wiley
p. 1379 - 1380
(2007/10/02)
More Articles about upstream products of 86008-21-1