Anchor Dependency for Non-Glycerol Based Cationic Lipofectins: Mixed Bag of Regular and Anomalous Transfection Profiles
摘要:
Although detailed structure activity, physicochemical and biophysical investigations in probing the anchor influence in liposomal gene delivery have been reported for glycerol-based transfection lipids, the corresponding investigation for non-glycerol based simple monocationic transfection lipids have not yet been undertaken. Towards this end, herein, we delineate our structure - activity and physicochemical approach in deciphering the anchor dependency in liposomal gene delivery using fifteen new structural analogues (lipids 1 - 15) of recently reported nonglycerol based monocationic transfection lipids. The C-14 analogues in both series 1 (lipids 1 - 6) and series 2 (lipids 7-15) showed maximum efficiency in transfecting COS-1 and CHO cells. However, the C-12 analogue of the ether series (lipid 3) exhibited a seemingly anomalous behavior compared with its transfection efficient C-10 and C-14 analogues (lipids 2 and 4) in being completely inefficient to transfect both COS-1 and CHO cells. The present structure - activity investigation also convincingly demonstrates that enhancement of transfection efficiencies through incorporation of membrane reorganizing unsaturation elements in the hydrophobic anchor of cationic lipids is not universal but cell dependent. The strength of the interaction of lipids 1 - 15 with DNA was assessed by their ability to exclude ethidium bromide bound to the DNA. Cationic lipids with long hydrophobic tails were found, in general, to be efficient in excluding EtBr from DNA. Gel to liquid crystalline transition temperatures of the lipids was measured by fluorescence anisotropy measurement technique. In general (lipid 2 being an exception), transfection efficient lipids were found to have their mid transition temperatures at or below physiological temperatures (37degreesC).
正确理解自组装过程对于在具有功能分子的2D表面上定制纳米结构的顺序至关重要。光致变色化合物是高级光响应性表面构件的有希望的候选者。为了研究分子结构与有序形成机理之间的关系,合成了通过酰胺基或酯基连接的各种长度的烷基侧链的2-噻吩基型二蒽。通过扫描隧道显微镜(STM)研究了它们在液体/固体界面的自组装。成核平衡常数(:表面覆盖的浓度依赖性通过使用合作模式为基于两个特征参数2D表面分析ķ Ñ)和伸长率平衡常数(K e)。可以得出以下结论。1)通过STM观察到稳定的2D分子有序排列的浓度随着烷基链长度的增加呈指数下降。2)带有酰胺基的化合物比带有酯基的化合物在2D表面上具有更高的自组装性(即σ,定义为K n / K e)。3)酯衍生物的开环异构体的自组装过程接近等当性,而闭环异构体的自组装过程是协作的,因为成核步骤的平衡常数不同(即,K n)之间的两个异构体。
Mononuclear iron complex and organic synthesis reaction using same
申请人:KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
公开号:US10363551B2
公开(公告)日:2019-07-30
A mononuclear iron bivalent complex having iron-silicon bonds, which is represented by formula (1), can exhibit an excellent catalytic activity in at least one reaction selected from three reactions, i.e., a hydrosilylation reaction, a hydrogenation reaction and a reaction for reducing a carbonyl compound.
(In the formula, R1 to R6 independently represent a hydrogen atom, an alkyl group which may be substituted by X, or the like; X represents a halogen atom, or the like; L1 represents at least one two-electron ligand selected from an isonitrile ligand, an amine ligand, an imine ligand, a nitrogenated heterocyclic ring, a phosphine ligand, a phosphite ligand and a sulfide ligand, wherein, when multiple L1's are present, two L1's may be bonded to each other; L2 represents a two-electron ligand that is different from a CO ligand or the above-mentioned L1, wherein, when multiple L2's are present, two L2's may be bonded to each other; and m1 represents an integer of 1 to 4 and m2 represents an integer of 0 to 3, wherein the sum total of m1 and m2 (i.e., m1+m2) satisfies 3 or 4.)
MONONUCLEAR IRON COMPLEX AND ORGANIC SYNTHESIS REACTION USING SAME
申请人:KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
公开号:US20160023196A1
公开(公告)日:2016-01-28
Provided is a mononuclear iron complex that comprises an iron-silicon bond that is represented by formula (1) and that exhibits excellent catalyst activity in each of a hydrosilylation reaction, a hydrogenation reaction, and reduction of a carbonyl compound.
In formula (1), R
1
-R
6
either independently represent an alkyl group, an aryl group, an aralkyl group or the like that may be substituted with a hydrogen atom or X, or represent a crosslinking substituent in which at least one pair comprising one of R
1
-R
3
and one of R
4
-R
6
is combined. X represents a halogen atom, an organoxy group, or the like. L represents a two-electron ligand other than CO. When a plurality of L are present, the plurality of L may be the same as or different from each other. When two L are present, the two L may be bonded to each other. n and m independently represent an integer of 1 to 3 with the stipulation that n+m equals 3 or 4.
PROCESS FOR PREPARING AMINES BY HOMOGENEOUSLY CATALYZED ALCOHOL AMINATION IN THE PRESENCE OF A COMPLEX CATALYST COMPRISING IRIDIUM AND AN AMINO ACID
申请人:BASF SE
公开号:US20140046054A1
公开(公告)日:2014-02-13
The invention relates to a process for preparing amines (A) by alcohol amination of alcohols (Al) by means of an aminating agent (Am) with elimination of water, wherein the alcohol amination is carried out in the presence of a complex catalyst comprising iridium and an amino acid.
ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
申请人:BEIJING INNOCARE PHARMA TECH CO., LTD.
公开号:US20190210997A1
公开(公告)日:2019-07-11
The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.