《抗肿瘤药》PPT课件-精选文档.ppt
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1、1,SECTION 1 Introduction(概述) SECTION 2 Agents directly acting on DNA (作用于DNA的药物) SECTION 3 Agents interfering with DNA synthesis (干扰DNA合成的药物) SECTION 4 Antimitotic agents (抗有丝分裂的药物) SECTION 5 New targets for antineoplastic agents (抗肿瘤药物的新靶点),2,SECTON 1 Introduction,neoplasm(肿瘤) The medical term for
2、cancer or tumor is neoplasm(肿瘤), which means “a relatively autonomous growth of tissue.” Tumor is a general term indicating any abnormal mass or growth of tissue, not necessarily life-threatening. A “cancerous tumor” is a malignant neoplasm with potential danger.,3,sarcoma In the early embryo of a m
3、ulticellular organism before organs begin to form, cells arrange themselves in three layersectodermal, mesodermal, and endodermal. Mesodermal cells form bone, muscle, cartilage, and related tissues.A cancer that arises from mesodermal tissue is called sarcoma. .,4,carcinoma Ectodermal cells form ski
4、n, its appendages, and nerve tissue. Endodermal cells form the intestinal system and its associated organs A cancer arises from ecto- or endodermal cells is called a carcinoma.,5,Blastoma The suffix-blastomais used to indicate certain types of tumors that have primitive appearance resembling embryon
5、ic structures. Cancers of blood A cancer of the blood involving abnormal increase of leukocytes is called leukemia.,6,Cell growth cycles,In a cells nucleus, DNA replication occurs during only one specific part of the cell cycle, called S for synthesis. Between division and S is a period called G1 in
6、 which cells grow, but do not make DNA. In G1, many molecules such as enzymes are synthesized. Another period called G2 occurs between S and the period called M, during which the two DNA copies separate.,7,Although each of these four main periods of the cell cycle (G1, S, G2, M) is unique, all in pr
7、oper order are necessary for new cell production. Normal and cancer cells behave differently. Normal cell: G1 G0 G1 Cancer cell: G1, S, G2, M G0 die,8,9,SECTON 2 Agents directly acting on DNA (作用于DNA的药物),I Alkylating agents (烷化剂) II Platinum Complex (金属铂配合物) III Bleomycin (博来霉素类) IV 作用于DNA拓扑异构酶(topo
8、ismerase)的药物,10,I Alkylating agents,Alkylating agents are reactive compounds that act on DNA, RNA, and certain enzymes. 1. Nitrogen mustards 2. Aziridines 3. Methanesulfonate esters and multiple alcohols 4. Nitrosoureas 5. Triazemylimidazole 6. Hydrazine derivatives),11,I Alkylating agents (烷化剂),1.
9、Nitrogen mustards(氮芥类) 载体部分 烷基化部分,12,Mechanism of nitrogen mustards,13,14,Many derivatives of the nitrogen mustards have been synthesized with various improvements. These agents are thought to react with 7 position of guanine in each of the double strands of DNA, causing cross-linking, which interfe
10、res with separation of the strands and prevents mitosis.,15,The principle use of mechlorethamine is in combination chemotherapy of Hodgkins disease and the non-Hodgkins lymphomas. It has wide activity, but more recent agents are safer and easier to use. A major disadvantage ultimately carcinogenic,
11、effect on bone marrow stem cells, culminating in a form of acute myelogenous leukemia.,Mechlorethamine Hydrochloride (盐酸氮芥),Mechlorethaminoxide Hydrochloride(盐酸氧氮芥),*,16,Chlorambucil Chlorambucil is used chiefly in chronic lymphocytic leukemia, usually orally because of its favorable aqueous solubil
12、ity as the sodium salt and rapid conversion to the free drug. Side effects are anorexia厌食, nausea, and vomiting.,17,*Melphalan It is effective in multiple myeloma(骨髓瘤)and has had a role in the treatment of breast and ovarian cancers. *Formylmerphalan ()-N-Formyl-4-bis-(b-chloroethyl)amino-phenylalan
13、ine (国产)降低毒性,18,Synthetic route of nitrogen mustards,19,*Cyclophosphamide (环磷酰胺) N,N-Bis(2-chloroethyl)tetrahydro-2H-1,3,2- oxazaphosphorin-2-amine-2-oxide monohydrate,20,Ifosfamide (异环磷酰胺) Trofosfamide (曲磷胺),21,2. Aziridines (乙撑亚胺类),Tretamine Hexamethylmelamine (Triethylenemelamine, (HMM, 六甲蜜胺) TEM
14、,三曲他胺,三乙蜜胺),p472,22,Tepa *Thiotepa (替哌) (塞替哌),23,*Mitomycin C (丝裂霉素C) Mitomycin C contains three groups that can damage cells: the quinone that can participate in free radical reactions generating superoxides, and aziridinyl and urethane(乌拉坦,氨基甲酸乙酯).,24,Reaction scheme for bioreductive activation of
15、 mitomycin C and the subsequent interstrand cross- linking of DNA.,25,3. Methanesulfonate esters and multiple alcohols (甲磺酸酯及多元醇类),*Busulfan (白消安,马利兰) 双功能的烷化剂,临床对于慢性粒细胞白血病的疗效显著,26,Dibromomannitol Dibromodulcilol (二溴甘露醇) (DBD, 二溴卫矛醇),Dianhydrogalactitol (DAG, 脱水卫矛醇): R=H Diacetyl dianhydrogalactitol
16、(DADAG, 脱水卫矛醇双乙酰化物): R=-COCH3,27,*Carmustine, BCNU(卡莫司汀,卡氮芥),N,N-Bis(2-chloroethyl)-N-nitrosourea,4. Nitrosoureas(亚硝基脲类),28,* Synthetic route of Carmustine (BCNU,卡莫司汀,卡氮芥),29,Lomustine (CCNU, 洛莫司汀) : R= Semustine (Me-CCNU,司莫司汀) : R= Nimustine (ACNU,盐酸尼莫司汀) : R= Ranimustine (雷莫司汀): R=,30,Decompositio
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