Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
摘要:
Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models. (C) 1999 Elsevier Science Ltd. ALI rights reserved.
Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
摘要:
Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models. (C) 1999 Elsevier Science Ltd. ALI rights reserved.
Persistent radical anions in the series of peri-arylenes: broadband light absorption until far in the NIR and purely organic magnetism
作者:Heinz Langhals、Ulrike Ritter-Faizade、Philipp Stadler、Marek Havlicek、Alexander Hofer、Niyazi Serdar Sariciftci
DOI:10.1007/s00706-019-02404-8
日期:2019.5
AbstractStable radicals in organic conjugated molecules are of great interest due to their magnetic signals and broad optical absorptions. In this paper, we report on naphthalene, benzoperylene, perylene, terrylene, and quaterrylene carboximides, reduced under controlled conditions, where stable metal-free solid salts of radical anions could be obtained forming darkly colored solutions with line-rich
The formula (I):
wherein each of R
2
and R
3
is, same or different, C2-C4 alkyl or the like; or R
2
and R
3
are taken together with the adjacent carbon atom to form a 5 to 8 membered non-aromatic carbocyclic ring; R
4
is C1-C6 alkyl or the like; X is an oxgen atom or a sulfur atom; A is the group of the formula:
wherein R
1
is, same or different, alkyl or the like; W is C2-C6 alkylene which may contain an optionally substituted heteroatom(s) or the like; n is an integer of 0 to 7, a pharmaceutically acceptable salt, or a solvate thereof.
The formula (I):
wherein each of R2 and R3 is, same or different, C2-C4 alkyl or the like; or R2 and R3 are taken together with the adjacent carbon atom to form a 5 to 8 membered non-aromatic carbocyclic ring; R4 is C1-C6 alkyl or the like; X is an oxgen atom or a sulfur atom; A is the group of the formula:
wherein R1 is, same or different, alkyl or the like; W is C2-C6 alkylene which may contain an optionally substituted heteroatom(s) or the like; n is an integer of 0 to 7, a pharmaceutically acceptable salt, or a solvate thereof.