JPS6034983A - Novel platinum complex - Google Patents
Novel platinum complexInfo
- Publication number
- JPS6034983A JPS6034983A JP14340683A JP14340683A JPS6034983A JP S6034983 A JPS6034983 A JP S6034983A JP 14340683 A JP14340683 A JP 14340683A JP 14340683 A JP14340683 A JP 14340683A JP S6034983 A JPS6034983 A JP S6034983A
- Authority
- JP
- Japan
- Prior art keywords
- cis
- alkyl
- trans
- amcha
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Abstract
Description
【発明の詳細な説明】
本発明は新規な白金錯体に関する。本発明に〔式中Ｂは
炭素数１−５のアルキル基を表わす。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to novel platinum complexes. In the present invention, B represents an alkyl group having 1 to 5 carbon atoms.
また、１−アミノメチル−アルキルシクロヘキシルアミ
ン（以下、アルキルａｍｃｈａともいう）の立体配位は
トランス−またはシス−を表わ鳴〕で表わされる白金錯
体〔以下、化合物（Ｉ）ともいう〕が提供される。In addition, a platinum complex [hereinafter also referred to as compound (I)] represented by 1-aminomethyl-alkylcyclohexylamine (hereinafter also referred to as alkyl amcha) whose configuration is trans- or cis- is provided. be done.
化合物（１）は抗菌活性、抗腫瘍活性を有し、医薬とし
、て有用である。Compound (1) has antibacterial activity and antitumor activity and is useful as a medicine.
種々の白金錯体が知られていて、それらが抗腫瘍活性を
有することも知られている。優れた抗腫瘍活性を有する
化合物はいつもめられておシ、この目的のため研究の結
果、全く新しい構造を有する化合物（１）が抗腫瘍活性
を有することを見出し、本発明を完成した。Various platinum complexes are known and it is also known that they have antitumor activity. Compounds with excellent antitumor activity are always sought after, and as a result of research for this purpose, it was discovered that compound (1) having a completely new structure has antitumor activity, and the present invention was completed.
上記化合物（１）において、Ｒの例としては、メチル、
エチル、グロビル等を包含する。In the above compound (1), examples of R include methyl,
Includes ethyl, globil, etc.
本化合物は、たとえば次の方法で製造することができる
。The present compound can be produced, for example, by the following method.
（１） ）ランスまたはシスアルキルａｍｅｈａ・２Ｈ
（ＪとＫｚＰｔ（１）Ｃ１４とを水性溶媒中で反応させ
、ｐｔ（Ｉ［）（Ｊ２（）ランスまたはシスアルキルａ
ｍｃｈａ ）を得る（ Ｂｕｌｌ、 Ｇｈｅｍ、 Ｓａ
ｃ、 Ｊｐｎ、。(1)) Lance or cis alkyl ameha・2H
(J and KzPt(1)C14 are reacted in an aqueous solvent, pt(I[)(J2() lance or cis alkyl a
mcha) get (Bull, Ghem, Sa
c, Jpn,.
社、 、４４９−４５４ （１９８３） 参照〕。See, Inc., 449-454 (1983)].
（２） ｔｌ＞で得られたＰｔ（ＩＩ）Ｃ：Ａ！ｇ （
） ’）シスまたはシスアルキルａｍｃｈａ ）とＡｇ
ＮＣ１ｇとを水性溶媒中、遮光下に反応させ、Ｐｔ（Ｉ
ｆ）（ＮＯｓｈ（）ランスまたはシスアルギルａｍｅｈ
ａ ）を得る□（３） Ｔ２）で得られたＰｔ（Ｉｌｌ
（ＮＯａ）ｚ（）ランスまたはシスアルキルａｍｃｈａ
）とマロン酸塩とを水性溶媒中で反応させ、結晶とし
て目的物、Ｐｔ１）（マロネー））（）？シスまたはシ
スアルキル為ｎ１ｃｈａ ）を得る。(2) Pt(II)C obtained with tl>:A! g (
) ') cis or cis alkyl amcha ) and Ag
1 g of NC was reacted in an aqueous solvent under light shielding to form
f) (NOsh() lance or cis-argyl ameh
a) Obtain □(3) Pt(Ill) obtained in T2)
(NOa)z() lance or cis alkyl amcha
) and malonate are reacted in an aqueous solvent to form the target product, Pt1) (Malonay)) ()?, in an aqueous solvent. For cis or cis alkyl, n1cha) is obtained.
化合物（１）の具体例およびその元素分析値を第１表に
示す。Specific examples of compound (1) and their elemental analysis values are shown in Table 1.
第１表 次に化合物（Ｉ）の抗腫瘍活性について示す。Table 1 Next, the antitumor activity of compound (I) will be shown.
ＣＤＦ マウス（１群６匹）にＬ １２１０の１０５個
の細胞を腹腔内投与し、投与当日、５白目１９日目に供
試化合物を投与し、平均生存期間の延長（Ｔ／Ｃ％）を
めた。結果を第２表に示す０第 ２ 表
以下に実施例を示す。10 cells of L 1210 were intraperitoneally administered to CDF mice (6 mice per group), and the test compound was administered on the 19th day of the 5th white of the eyes on the day of administration to increase the mean survival period (T/C%). I met. The results are shown in Table 2. Examples are shown below in Table 2.
実施例１
ｄＪｌ！−）；ｙ／Ｘ−２メチルａｍｅｈａ−２Ｈ（Ｊ
／２．１６１ （０，０１モル）を５０−の水に、ま
たに２Ｐｔ（Ｊ１４４．１７．９ （０，０１モル）を
５ｄの水に溶解し、両者を混合、放置すると淡黄色のＰ
ｔＣ４ｚ（ａｌ−）ランス−２メチルａｍｃｈａ ）の
結晶性沈殿が得られる。Example 1 dJl! -); y/X-2 methyl ameha-2H (J
/2.161 (0.01 mol) is dissolved in 50-water and 2Pt (J144.17.9 (0.01 mol) is dissolved in 5-d water. When the two are mixed and left to stand, a pale yellow Pt.
A crystalline precipitate of tC4z(al-) lance-2 methyl amcha) is obtained.
ついで得られたＰｔＧｌｚ （ｄｌ−）ランス−２メチ
ルａｍｃｈａ ） ４．０９１ （０，０１モル）をＡ
ｇＮＯｓ ３．４０＃（０，０２モル）と１００１の水
に懸濁させ、アルミ箔で遮光し、３−７日間ｋｇｃ；ｌ
が完全に析出す（ｄ７−ト２／スー２メチＡ／ ａｍｃ
ｈａ ）が得られる。Then, the obtained PtGlz (dl-) lance-2 methyl amcha) 4.091 (0.01 mol) was converted into A
Suspend gNOs 3.40 # (0.02 mol) in 1001 water, shield from light with aluminum foil, and leave kgc; l for 3-7 days.
completely precipitates (d7-t2/su2methyA/amc
ha) is obtained.
得られたＰｔ（ＣＯａ）２（ｄノー トランス−２メチ
ルａｍａｈａ ） ４．６１１ （０，０１モル）とマ
ロン酸ナトリウム１．３４ｊ’ （０，０１モル）を水
１ｏｏ ｍｌに加温溶解し、−夜装置すると白色結晶の
Ｐｔ（マロネート）（ｄｉ−トランス−２メチルａｍｅ
ｈａ ） （化合物・１）が得られる。The obtained Pt(COa)2(d-no-trans-2-methyl-amaha) 4.611 (0.01 mol) and sodium malonate 1.34j' (0.01 mol) were dissolved by heating in 10 ml of water, - When used at night, white crystals of Pt (malonate) (di-trans-2 methyl ame) appear.
ha) (Compound 1) is obtained.
実施例２−４
実施例１においてｄＪ−）ランス−２メチルａｍａｈａ
・２ＨｃＪ の代わシに、ｄｌ−シス−３メチルａｍｅ
ｈｍ・２ＨＧ７、トランス−４メチルａｍｏｈａ・２Ｈ
Ｃノおよびシス−４メチルａｍｃｈａ・２ＨＣノ を用
いる以外は実施例１と同様にして、化合物２．３および
４を得る〇Example 2-4 In Example 1, dJ-) lance-2 methyl amaha
・In place of 2HcJ, dl-cis-3 methyl ame
hm・2HG7, trans-4 methyl amoha・2H
Compounds 2.3 and 4 are obtained in the same manner as in Example 1 except for using C and cis-4 methyl amcha.2HC.
第１図および第２図はマロネー） （ｄＪ−）ランス−
１−アミノメチル−２−メチルシクロヘキシルアミン）
白金（Ｉｌｌおよびマロネート（シス−１−アミノメチ
ル−４−メチルシクロヘキシルアミン）白金（Ｉｔ）の
赤外綜吸収スペクトルを示すＯ
特許出願人 喜 谷 喜 徳Figures 1 and 2 are Maroney) (dJ-) Lance-
1-aminomethyl-2-methylcyclohexylamine)
O showing the infrared absorption spectrum of platinum (Ill and malonate (cis-1-aminomethyl-4-methylcyclohexylamine) platinum (It)) Patent applicant Yoshinori Kitani
Claims (1)
ンの立体配位はトランス−またはシス−を表わす。）で
表わされる白金錯体。[Claims] General formula (1) (In the formula, R represents an alkyl group having 1 to 5 carbon atoms. Also, the configuration of 1-aminomethyl-alkylcyclohexylamine represents trans- or cis-.) A platinum complex represented by
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP14340683A JPS6034983A (en) | 1983-08-05 | 1983-08-05 | Novel platinum complex |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP14340683A JPS6034983A (en) | 1983-08-05 | 1983-08-05 | Novel platinum complex |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS6034983A true JPS6034983A (en) | 1985-02-22 |
Family
ID=15338027
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP14340683A Pending JPS6034983A (en) | 1983-08-05 | 1983-08-05 | Novel platinum complex |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6034983A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6087295A (en) * | 1983-10-19 | 1985-05-16 | Nippon Kayaku Co Ltd | Novel platinum complex |
| US4748254A (en) * | 1984-01-23 | 1988-05-31 | Institut Obschei I Neorganicheskoi Khimii Imeni N.S. Kurnakova Akademii Nauk SSR | Mixed carboxylato platinum (II) complexes |
-
1983
- 1983-08-05 JP JP14340683A patent/JPS6034983A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6087295A (en) * | 1983-10-19 | 1985-05-16 | Nippon Kayaku Co Ltd | Novel platinum complex |
| JPH0412277B2 (en) * | 1983-10-19 | 1992-03-04 | Nippon Kayaku Kk | |
| US4748254A (en) * | 1984-01-23 | 1988-05-31 | Institut Obschei I Neorganicheskoi Khimii Imeni N.S. Kurnakova Akademii Nauk SSR | Mixed carboxylato platinum (II) complexes |
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